signal transducer and activator of transcription

The signal transducer and activator of transcription 6 fragments is a peptide with the sequence H2N-Ser-Tyr-Trp-Ser-Asp-Arg-Leu-Ile-Ile-OH, MW= 1152.3.

7-Bromohept-1-yne is a PROTAC Linker that can be used to synthesize AK-1690, a STAT6 (Signal transducer and activator of transcription 6) PROTAC degradator.

DB-381831 is an organic phosphorus compound with a complex molecular structure that includes a benzothiophene ring, carboxyl group, diethoxyphosphoryl group, and difluoromethyl group. It may be used as an important intermediate or reagent in organic synthesis reactions. DB-381831 is involved in the synthesis of AK-2292, a STAT5 (Signal transducer and activator of transcription 5) small molecule degradator.

STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.

STAT3/AKT-IN-1 is a dual inhibitor of the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signaling pathways, demonstrating anti-tumor activity and inducing apoptosis in SGC-7901 cells.

STAT6-IN-10 is a highly active signal transducer and activator of transcription 6 (STAT6) inhibitor with an EC₅₀ of 0.002 μM. It inhibits the secretion of CCL17 in human peripheral whole blood with an IC₅₀ of 0.095 μM and can be used in research on skin diseases and respiratory disorders.

STAT3-IN-46 is a selective, orally active inhibitor of the signal transducer and activator of transcription 3 (STAT3), with a KD value of 323.3 nM. It binds directly to the SH2 domain of STAT3, inhibiting the IL-6/JAK/STAT3 signaling pathway with an IC50 value of 0.87 μM, and decreases levels of c-Myc and Bcl-2. STAT3-IN-46 is applicable in cancer research, including studies on triple-negative breast cancer.

STAT3-IN-52 (Compound 9) is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3). It binds to the pY705 site of STAT3 with a Ki of 440 nM, effectively hindering STAT3 phosphorylation and dimerization. STAT3-IN-52 exhibits potent cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 of 0.7 μM), medulloblastoma UW426, and pancreatic cancer BKPC3 cells. The compound induces apoptosis, inhibits STAT3's nuclear translocation and DNA-binding activity, and downregulates the expression of the STAT3 target gene MMP9. STAT3-IN-52 is useful in research related to cancers with aberrant STAT3 activation.

HJC0149 is a potent orally bioavailable signal transducer and activator of transcription 3 inhibitor.

HJC0416 is a potent orally bioavailable signal transducer and activator of transcription 3 inhibitor.

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

HJC0152 hydrochloride (HJC0152) is a signal transducer and activator of transcription 3 (STAT3) inhibitor.

Brivudine monophosphate is a phosphate ester of Brivudine. Brivudine, also known as bromovinyl-deoxyuridine, is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator of transcription 3), which may result in the downregulation of vascular endothelial growth factor (VEGF). BVDU has also been found to inhibit the upregulation of chemoresistance genes (Mdr1 and DHFR) during chemotherapy.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Falbikitug is a humanized IgG1 monoclonal antibody targeting leukemia inhibitory factor (LIF). it inhibits downstream signaling by specifically blocking the recruitment of the glycoprotein 130 (gp130) coreceptor to the LIF receptor (LIFR) subunit (gp190), consequently preventing the phosphorylation of signal transducer and activator of transcription 3 (STAT3), and is intended for treating advanced solid tumors.

Ganoderic acid A (Standard) is a reference standard for research and analysis in studies involving Ganoderic acid A. 1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human osteosarcoma HOS and MG-63 cells. 3. Ganoderic acid A promotes cisplatin-induced cell death by enhancing the sensitivity of HepG2 cells to cisplatin mainly via the signal transducer and activator of transcription 3 suppression, significantly suppresses IL-6-induced signal transducer and activator of transcription 3 phosphorylation.

Manassantin B (Standard) is a reference standard for research and analysis in studies involving Manassantin B. Manassantin B is a potent inhibitor of NF-κB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-κB. It also possesses anti-EBV lytic replication activity. Manassantin B inhibits interleukin-6-induced signal transducer and activator of transcription 3 activation in Hep3B cells, it has potential as a potent anti-inflammatory drug for use in pathological processes such as sepsis or acute lung injury. Manassantin B exerts antifibrotic activity in HSC-T6 cells, in part, via inhibition of cell proliferation and decrease of collagen production.

Manassantin B is a potent inhibitor of NF-κB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-κB. It also possesses anti-EBV lytic replication activity. Manassantin B inhibits interleukin-6-induced signal transducer and activator of transcription 3 activation in Hep3B cells, it has potential as a potent anti-inflammatory drug for use in pathological processes such as sepsis or acute lung injury. Manassantin B exerts antifibrotic activity in HSC-T6 cells, in part, via inhibition of cell proliferation and decrease of collagen production.

Boscialin can inhibit signal transducer and activator of transcription 1 translocation at a concentration of 10 uM.